Purity & Documentation

References

GSK963 is significantly more potent than Nec-1 in both biochemical and cellular assays, inhibiting RIP1-dependent cell death with an IC50 of between 1 and 4 nM in human and murine cells. GSK963 is >10000-fold selective for RIP1 over 339 other kinases, lacks measurable activity against IDO and has an inactive enantiomer[1].

In Vivo

GSK963 provides complete protection in an in vivo model of TNF-induced sterile shock at a dose where Nec-1 shows no significant protection in the model. Treatment of animals with 2 mg/kg of GSK963 results in a complete protection from TNF +zVAD-induced temperature loss, with the 0.2 mg/kg dose also showing a significant response[1].

Solvent & Solubility

In Vitro:

DMSO : 150 mg/mL (651.30 mM; Need ultrasonic)

Preparing Stock Solutions

ConcentrationSolventMass

1 mg

5 mg

10 mg

1 mM

4.3420 mL

21.7099 mL

43.4197 mL

5 mM

0.8684 mL

4.3420 mL

8.6839 mL

10 mM

0.4342 mL

2.1710 mL

4.3420 mL

*Please refer to the solubility information to select the appropriate solvent.